2. Signaling Pathways
  3. Cell Cycle/DNA Damage
  4. Topoisomerase

Topoisomerase

Topoisomerase

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Topoisomerases are enzymes that regulate the overwinding or underwinding of DNA. The winding problem of DNA arises due to the intertwined nature of its double-helical structure. Topoisomerases are isomerase enzymes that act on the topology of DNA. Type I topoisomerase cuts one strand of a DNA double helix, relaxation occurs, and then the cut strand is reannealed. Type I topoisomerases are subdivided into two subclasses: type IA topoisomerases, which share many structural and mechanistic features with the type II topoisomerases, and type IB topoisomerases, which utilize a controlled rotary mechanism. Type II topoisomerase cuts both strands of one DNA double helix, pass another unbroken DNA helix through it, and then reanneal the cut strands. This class is also split into two subclasses: type IIA and type IIB topoisomerases, which possess similar structure and mechanisms.

Topoisomerase Isoform Specific Products:

Topoisomerase Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-118168
    A 9387
    		Inhibitor
    A9387 is an inhibitor of the Tn3 Resolvase, which promotes site-specific recombination reactions between two directly repeated recombination sites. Several inhibitors have been isolated that inhibit this event. A9387 inhibits the binding of resolvase to the res site.
    A 9387
  • HY-175269
    MGB1Y
    		Inhibitor
    MGB1Y is a noncovalent DNA minor groove binder (MGB). MGB1Y potently inhibits cancer cells proliferation and topoisomerase I activity. MGB1Y downregulates their breast cancer-related genes in MCF7 and MDA-MB-231 cells. MGB1Y has a broad-spectrum anticancer activity, such as breast cancer, colon cancer, and leukemia.
    MGB1Y
  • HY-135255
    NSC 660028
    		Inhibitor
    NSC 660028 is a DNA topoisomerase II (DNA topoisomerase II) inhibitor with an ID50 of 50 μM. NSC 660028 inhibits DNA topoisomerase II and induces protein-linked DNA breaks. NSC 660028 can be used for cancer research.
    NSC 660028
  • HY-183330
    Topo I/II-IN-3
    		Inhibitor
    Topo I/II-IN-3 is a dual inhibitor of topoisomerase I/II (topoisomerase I/II), with an IC50 of 8.99 μM against Topo I and an IC50 of 26.92 μM against Topo II. Topo I/II-IN-3 induces DNA damage, elevates intracellular ROS levels, activates the mitochondrial apoptosis pathway, and exerts cytotoxicity against cancer cells. Topo I/II-IN-3 upregulates the expression of γ-H2AX, p53, activated caspase-9, Bax and activated caspase-3, while downregulating the expression of Bcl-2. Topo I/II-IN-3 can be used in research related to breast cancer, liver cancer and gastric cancer.
    Topo I/II-IN-3
  • HY-171738
    Anti-SLC34A2 (Lifastuzumab)-MC-Vc-PAB-SN38
    		Inhibitor
    Anti-SLC34A2 (Lifastuzumab)-MC-Vc-PAB-SN38 is an antibody-drug conjugate (ADC) consisting of the humanized anti-SLC34A2 (sodium-dependent phosphate transporter 2) antibody Lifastuzumab (HY-P99970) conjugated to the linker Mc-VC-PAB and the topoisomerase I inhibitor SN38 (HY-13704). The ADC toxic molecule and linker part are Mc-VC-PAB-SN38 (HY-131057). Anti-SLC34A2 (Lifastuzumab)-MC-Vc-PAB-SN38 can be used in cancer research.
    Anti-SLC34A2 (Lifastuzumab)-MC-Vc-PAB-SN38
  • HY-163723
    EGFR-IN-116
    		Inhibitor
    EGFR-IN-116 (compound 14D) is an anticancer agent. EGFR-IN-116 against EGFR has the IC50 values​of EGFR, VEGFR-2 and Topo II are 0.103 μM, 0.069 μM and 19.74 μM, respectively.
    EGFR-IN-116
  • HY-173703
    β-Glu-PAB(CH2NH2)-Exatecan
    		Inhibitor
    β-Glu-PAB(CH2NH2)-Exatecan (Compound 9a) is a topoisomerase I inhibitor. β-Glu-PAB(CH2NH2)-Exatecan binds to the topoisomerase I-DNA complex to prevent DNA strand reconnection, thereby inducing DNA breakage and cell apoptosis. β-Glu-PAB(CH2NH2)-Exatecan can be specifically cleaved by β-glucuronidase highly expressed in the tumor microenvironment to release Exatecan for cytotoxic effect. β-Glu-PAB(CH2NH2)-Exatecan is also an intermediate of Mal((3S,3aR,6S,6aR) -hexahydrofuro [3, 2-B]furan-3,6-diamine-PEG12)-β -Glu-Pab-Exatecan. β-Glu-PAB(CH2NH2)-Exatecan is promising for research of cancers.
    β-Glu-PAB(CH2NH2)-Exatecan
  • HY-203913
    Topoisomerase I-IN-19
    		Inhibitor
    Topoisomerase I-IN-19 (Example 36) is a Topoisomerase I inhibitor. Topoisomerase I-IN-19 can be used to investigate Topoisomerase I-mediated diseases such as cancer.
    Topoisomerase I-IN-19
  • HY-145852
    Top/HDAC-IN-2
    		Inhibitor
    Top/HDAC-IN-2 (45b), a Top and HDAC dual inhibitor, exhibits potent antitumor activities and induces apoptosis.
    Top/HDAC-IN-2
  • HY-B0356G
    Ciprofloxacin (GMP)
    		Inhibitor
    Ciprofloxacin GMP is Ciprofloxacin (HY-B0356) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Ciprofloxacin (Bay-09867) is an orally active, blood-brain barrier permeable fluoroquinolone antibacterial agent. Ciprofloxacin exerts bactericidal effects primarily by inhibiting topoisomerase II and IV. Ciprofloxacin inhibits the proliferation of human dental pulp stem cells and chondrocytes from young rats, and also activates the Akt signaling pathway and upregulates markers such as β-catenin and Nanog to maintain the morphological characteristics of stem cells. Ciprofloxacin induces significant neurotoxicity and tissue damage, including reducing serotonin and glutathione levels in the brain, inducing oxidative stress and depression-like behaviors, and causing articular cartilage damage. Ciprofloxacin can be applied to research related to infections of necrotic young permanent teeth and neurotoxicity.
    Ciprofloxacin (GMP)
  • HY-149271
    Anti-MRSA agent 7
    		Inhibitor
    Anti-MRSA agent 7 (Compound 12) is a potent antibacterial agent. Anti-MRSA agent 7 inhibits S. aureus DNA gyrase, E. coli DNA gyrase, S. aureus topo IV and E. coli topo IV with IC50s of 0.185, 0.365, 0.341 and 0.059 μM, respectively.
    Anti-MRSA agent 7
  • HY-177678
    N-(Azido-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan)
    N-(Azido-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan) is a drug-linker conjugate for ADC (Drug-Linker Conjugate for ADC), consisting of a tubulin polymerization inhibitor MMAE (HY-15162) and a DNA topoisomerase I inhibitor Exatecan (HY-13631), and an ADC linker composition. N-(Azido-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan) can be used for synthesis of ADCs and for cancer research.
    N-(Azido-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan)
  • HY-162380
    Topoisomerase II inhibitor 18
    		Inhibitor
    Topoisomerase II inhibitor 18 (Compound IV) is a Quinoxaline derivative, which inhibits topoisomerase II with IC50 of 7.5 μM. Topoisomerase II inhibitor 18 inhibits proliferation, cell cycle at S phase and induces apoptosis in PC-3 cells. Topoisomerase II inhibitor 18 reveals antitumor activity against cancer.
    Topoisomerase II inhibitor 18
  • HY-W654323
    PNU-142586 sodium
    		Inhibitor
    PNU-142586 sodiu) is the major metabolite of Linezolid (HY-10394). PNU-142586 can inhibit the activity of DNA topoisomerase 2-α (TOP2A) and DNA topoisomerase 2-β (TOP2B). PNU-142586 interferes with DNA replication and transcription by blocking the binding of DNA to TOP2 and inhibiting ATP hydrolysis, ultimately leading to antiproliferative and cytotoxic effects, including mitochondrial dysfunction. PNU-142586 can be used to study Linezolid-induced hematotoxicity and its molecular mechanism.
    PNU-142586 sodium
  • HY-168739
    Topoisomerase I inhibitor 17
    		Inhibitor
    Topoisomerase I inhibitor 17 (Compound 7h) is a Topoisomerase I (Top1) inhibitor. Topoisomerase I inhibitor 17 reduces DDX5 and reverses the locking of Top1 activity by DDX5. Topoisomerase I inhibitor 17 induces Top1-mediated DNA damage and promotes reactive oxygen species (ROS) production. Topoisomerase I inhibitor 17 induces Apoptosis (reduces antiapoptotic proteins XIAP, Bcl-2, Survivin and up-regulates pro-apoptotic proteins Bax, γH2AX). Topoisomerase I inhibitor 17 also blocks the progression of the G2/M checkpoint and induces cell cycle arrest. Topoisomerase I inhibitor 17 significantly inhibits colony formation and cell migration in colorectal cancer cells. Topoisomerase I inhibitor 17 effectively reduces tumors in human PDX tumor mice.
    Topoisomerase I inhibitor 17
  • HY-N0498R
    Nitidine chloride (Standard)
    		Inhibitor
    Nitidine (chloride) (Standard) is the analytical standard of Nitidine (chloride). This product is intended for research and analytical applications. Nitidine chloride, a potential anti-malarial lead compound derived from Zanthoxylum nitidum (Roxb) DC, exerts potent anticancer activity through diverse pathways, including inducing apoptosis, inhibiting STAT3 signaling cascade, DNA topoisomerase 1 and 2A, ERK and c-Src/FAK associated signaling pathway. Nitidine chloride inhibits LPS-induced inflammatory cytokines production via MAPK and NF-kB pathway.
    Nitidine chloride (Standard)
  • HY-143279
    Topoisomerase II inhibitor 3
    		Inhibitor
    Topoisomerase II inhibitor 3 (Compound 6 h ) is a acridone derivatives, as well as a Type II DNA topoisomerase (topo II) inhibitor , as a topo IIα/β inhibitor with the value of IC50 is 0.17 μM for topo IIα and the value of IC50 is 0.23 μM for topo IIβ subtypes, caused obvious DNA damage, and induced apoptosis by triggering the loss of mitochondrial membrane potential.
    Topoisomerase II inhibitor 3
  • HY-116933
    Murrayanol
    		Inhibitor
    Murrayanol is a natural carbazole alkaloid with a variety of biological activities. Murrayanol shows anti-inflammatory, topoisomerase I and topoisomerase II (Topoisomerase) inhibition activities. Murrayanol also as a mosquitocidal and antimicrobial.
    Murrayanol
  • HY-13726
    Piroxantrone
    		Inhibitor
    Piroxantrone (Oxantrazole) is a potent DNA topoisomerase II-targeting anthrapyrazole antitumor agent. Piroxantrone displays cardiotoxicity.
    Piroxantrone
  • HY-146316
    Topoisomerase II inhibitor 6
    		Inhibitor
    Topoisomerase II inhibitor 6 (Compound 5), a tryptanthrin derivative, is a potent and selective inhibitor of topoisomerase II. Topoisomerase II inhibitor 6 exhibits antiproliferative activity on different tumor cell lines. Topoisomerase II inhibitor 6 blocks the cell cycle of CCRF-CEM in the G2 phase and induces DNA DSB. Topoisomerase II inhibitor 6 has the potential for the research of cancer diseases.
    Topoisomerase II inhibitor 6
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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